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Ceftaroline Fosamil is a fifth-generation cephalosporin, a broad-spectrum β-lactam active against MRSA and respiratory pathogens.  Branded as Teflaro in the US and Zinforo in Europe, it is active against bacteria causing community-acquired pneumonia and complicated skin and skin structure infections.  Ceftaroline Fosamil is sparingly soluble in DMSO.

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    Mechanism of Action

    Ceftaroline Fosamil binds to penicillin-binding protein (PBP) which prevents the formation of the bacterial cell wall. MRSA strains have a mutated PBP2a which prohibits β-lactam antibiotics from accessing its active site.  Ceftaroline has an ethyoxyimino side-chain mimicking a portion of a cell wall structure, which opens and facilitates access to the active site of PBP2a.

    Ceftaroline Fosamil is a prodrug that is converted in vivo to active metabolite Ceftaroline (and inactive metabolite Ceftaroline-M1) by plasma phosphatases.  

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    Ceftaroline Fosamil is broad-spectrum against Gram-positive and Gram-negative bacteria. It is effective against methicillin-resistant Staphylococcus aureus (MRSA), and extensively-resistant strains such as vancomycin-resistant S. aureus (VRSA), vancomycin-intermediate S. aureus (VISA), and heteroresistant VISA (hVISA). It is also effective against respiratory pathogens like Streptococcus pneumoniae and Haemophilus influenzae.


    Microbiology Applications

    In vitro studies show a similar spectrum to ceftobiprole, the only other 5th generation cephalosporin to date. 

     Microbiology Applications

    Ceftaroline is commonly used in clinical in vitro microbiological antimicrobial susceptibility tests (panels, discs, and MIC strips).   Medical microbiologists use AST results to recommend antibiotic treatment options.  Representative MIC values include:

      • MRSA 0.5-2.0 µg/ml
      • MSSA 0.25 µg/ml
      • hVISA 0.25-4 µg/ml
      • For a representative list of Ceftaroline MIC values, click here.



    Biek D, Critchley IA, Riccobene TA and Thye DA (2010)  Ceftaroline fosamil: A novel broad-spectrum cephalosporin with expanded anti-Gram-positive activity.  J. Antimicrob. Chemother. 65(4):iv9-iv16  PMID 21115457

    Duplessis C and Crum-Cianflone NF  (2011) Ceftaroline: A new cephalosporin with activity against methicillin-resistant Staphylococcus aureus (MRSA). Clin. Med. Rev. Ther. 3. a2466. PMID  21785568

    Laudano, J (2011) Ceftaroline fosamil: a new broad-spectrum cephalosporin. J. Antimicrob. Chemother. 66(Supp. 3): iii11-iii18

    Saravolatz LD, Stein GE and Johnson LB (2011)  Ceftaroline: A novel cephalosporin with activity against methicillin-resistant Staphylococcus aureus.  Clin. Infect. Dis. 52(9):1156-1163  PMID 21467022

    Zhanel GC et al (2009)  Ceftaroline. Drugs 69(7):809-831

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